Assay Detail
Binding
CHEMBL829833
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Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.89 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66393 | — | — | 1 | 6.85 |
| CHEMBL307199 | — | — | 1 | 6.70 |
| CHEMBL191809 | — | — | 1 | 6.40 |
| CHEMBL2368364 | — | — | 1 | 6.37 |
| CHEMBL2368363 | — | — | 1 | 6.32 |
| CHEMBL193692 | — | — | 1 | 6.29 |
| CHEMBL331382 | METRIFUDIL | 2.0 | 1 | 6.12 |
| CHEMBL27376 | — | — | 1 | 6.11 |
| CHEMBL2368368 | — | — | 1 | 6.10 |
| CHEMBL417292 | — | — | 1 | 6.07 |
| CHEMBL2368369 | — | — | 1 | 6.07 |
| CHEMBL2368365 | — | — | 1 | 5.96 |
| CHEMBL353319 | — | — | 1 | 5.92 |
| CHEMBL2112156 | — | — | 1 | 5.89 |
| CHEMBL2368455 | — | — | 1 | 5.89 |
| CHEMBL193385 | — | — | 1 | 5.85 |
| CHEMBL2368366 | — | — | 1 | 5.80 |
| CHEMBL27809 | — | — | 1 | 5.80 |
| CHEMBL364671 | — | — | 1 | 5.64 |
| CHEMBL175543 | — | — | 1 | 5.64 |
| CHEMBL193421 | — | — | 1 | 5.60 |
| CHEMBL119709 | IB-MECA | — | 1 | 5.54 |
| CHEMBL2112160 | — | — | 1 | 5.43 |
| CHEMBL2112158 | — | — | 1 | 5.42 |
| CHEMBL2112163 | — | — | 1 | 5.32 |
| CHEMBL2112155 | — | — | 1 | 5.29 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 5.27 |
| CHEMBL280580 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66393 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL307199 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL191809 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL2368364 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL2368363 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL193692 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL331382 | METRIFUDIL | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL27376 | — | Ki | = | 784.0 | nM | 6.11 |
| CHEMBL2368368 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL417292 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL2368369 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL2368365 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL353319 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL2112156 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL2368455 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL193385 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2368366 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL27809 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL364671 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL175543 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL193421 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL119709 | IB-MECA | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL2112160 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL2112158 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL2112163 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL2112155 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL280580 | — | Ki | = | 6200.0 | nM | 5.21 |